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Journal of Cancer Prevention


J Cancer Prev 2020; 25(4): 213-222

Published online December 30, 2020

© Korean Society of Cancer Prevention

Recent Advances in the Development of TGF-β Signaling Inhibitors for Anticancer Therapy

Ho-Jae Lee

Department of Biochemistry, Lee Gil Ya Cancer and Diabetes Institute, Gachon University College of Medicine, Incheon, Korea

Correspondence to :
Ho-Jae Lee, E-mail:,

Received: December 1, 2020; Revised: December 13, 2020; Accepted: December 14, 2020


TGF-β is a multifunctional cytokine that plays an important role in both physiologic and pathologic processes, including cancer. Importantly, TGF-β has a dual role in tumorigenesis, acting as a tumor suppressor or a tumor promoter, depending on the stage of tumor development. The aberrantly upregulated production of TGF-β has been strongly implicated in tumor progression, angiogenesis, and metastasis, as well as immune evasion. Therefore, hyperactivated TGF-β signaling is considered a potential therapeutic target for cancer therapy. Numerous inhibitors of overactivated TGF-β signaling have been developed, and some of them are currently in clinical trials. This review focuses on the TGF-β signaling that contributes to tumor progression and immune evasion in the tumor microenvironment and presents recent achievements on TGF-β signaling inhibition as a single or combined therapeutic approach in cancer therapy.

Keywords: TGF-β, Tumor microenvironment, Tumor escape, Antineoplastic agents, Immune checkpoint inhibitors

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